Antibody-activation of connexin hemichannels in bone osteocytes with ATP release suppresses breast cancer and osteosarcoma malignancy

Cell Rep. 2024 Jul 23;43(7):114377. doi: 10.1016/j.celrep.2024.114377. Epub 2024 Jun 17.

Abstract

Bone tissue represents the most frequent site of cancer metastasis. We developed a hemichannel-activating antibody, Cx43-M2. Cx43-M2, directly targeting osteocytes in situ, activates osteocytic hemichannels and elevates extracellular ATP, thereby inhibiting the growth and migration of cultured breast and osteosarcoma cancer cells. Cx43-M2 significantly decreases breast cancer metastasis, osteosarcoma growth, and osteolytic activity, while improving survival rates in mice. The antibody's inhibition of breast cancer and osteosarcoma is dose dependent in both mouse and human cancer metastatic models. Furthermore, Cx43-M2 enhances anti-tumor immunity by increasing the population and activation of tumor-infiltrating immune-promoting effector T lymphocytes, while reducing immune-suppressive regulatory T cells. Our results suggest that the Cx43-M2 antibody, by activating Cx43 hemichannels and facilitating ATP release and purinergic signaling, transforms the cancer microenvironment from a supportive to a suppressive state. Collectively, our study underscores the potential of Cx43-M2 as a therapeutic for treating breast cancer bone metastasis and osteosarcoma.

Keywords: ATP; CP: Cancer; CP: Cell biology; Cx43 hemichannels; Cx43-M2; T cells; bone metastasis; breast cancer; osteosarcoma.

MeSH terms

  • Adenosine Triphosphate* / metabolism
  • Animals
  • Antibodies / pharmacology
  • Bone Neoplasms* / metabolism
  • Bone Neoplasms* / pathology
  • Bone Neoplasms* / secondary
  • Breast Neoplasms* / metabolism
  • Breast Neoplasms* / pathology
  • Cell Line, Tumor
  • Connexin 43* / metabolism
  • Female
  • Humans
  • Mice
  • Osteocytes* / metabolism
  • Osteosarcoma* / metabolism
  • Osteosarcoma* / pathology
  • Tumor Microenvironment

Substances

  • Adenosine Triphosphate
  • Connexin 43
  • Antibodies